新产品编号:2443117

Chemical Name: N-[3-[3-(4-Hydroxy-3,5-diisopropylphenyl)propylaminomethyl]phenyl]thiophene-2-carboxamidine dihydrochloride
项目整合开发状态: Biological Testing
项目研究机构: Ipsen (Originator)
合成路线:Reduction of N-Boc-3-nitrobenzylamine (I) by catalytic hydrogenation over Pd/C yields aniline (II).This is then condensed with S-methyl-2-thiophenethiocarboximide (III) to furnish amidine (IV).Subsequent acidic Boc group cleavage yields amine (V).

合成路线:3,5-Diisopropyl-4-hydroxybenzaldehyde (VI) is esterified with acetyl chloride,producing acetate (VII).Subsequent Wittig condensation of aldehyde (VII) with carboethoxymethylene triphenylphosphorane leads to the cinnamyl derivative (VIII),which is further hydrogenated to the arylpropionic ester (IX).After saponification of ester (IX) with LiOH,the resultant carboxylic acid (X) is coupled to amine (V),producing amide (XI).Finally,amide reduction with borane in THF gives rise to the target amine.